Inventors:
Roberta L. Dorow - Portage MI, 49024
Silvio Campagna - New Castle DE, 19720
Pasquale N. Confalone - Greenville DE, 19807
Fuqiang Jin - Wilmington DE, 19810
Zhe Wang - Hockessin DE, 19707
International Classification:
C07C23101
US Classification:
540456, 544168, 560169, 560172, 564135, 564136, 564139, 564143, 564153, 564158, 564159, 564205, 564207, 564208
Abstract:
The present invention is directed to a process for the preparation of a compound of formula (X-a) or a pharmaceutically acceptable salt form thereof, wherein: R is selected from the group consisting of: C alkyl substituted with 0-5 R , â(CH ) âC cycloalkyl substituted with 0-5 R , and â(CH ) -aryl substituted with 0-5 R. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.